Acta Pharm. 59 (2009) 45-55

full paper

Original research paper

Preclinical studies of [⁶¹Cu]ATSM as a PET radiopharmaceutical for fibrosarcoma imaging

AMIR R. JALILIAN, NIMA ROSTAMPOUR, PEJMAN ROWSHANFARZAD, KAMALEDDIN SHAFAII, MOHSEN KAMALI-DEHGHAN, MEHDI AKHLAGHI, MOHAMMAD B. TAVAKOLI

ajalilian@nrcam.org

¹Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research School (AMIRS), Karaj, Iran

²Department of Medical Physics, School of Medicine, University of Medical Sciences, Hamadan, Iran

Accepted February 3, 2009

[⁶¹Cu]diacetyl-bis(N⁴-methylthiosemicarbazone) ([⁶¹Cu]ATSM) was prepared using in house-made diacetyl-bis(N⁴-methylthiosemicarbazone) (ATSM) ligand and [⁶¹Cu]CuCl₂ produced via the ^natZn(p,x)⁶¹Cu (180 μA proton irradiation, 22 MeV, 3.2 h) and purified by a ion chromatography method. [⁶¹Cu]ATSM radiochemical purity was >98%, as shown by HPLC and RTLC methods. [⁶¹Cu]ATSM was administered into normal and tumor bearing rodents for up to 210 minutes, followed by biodistribution and co-incidence imaging studies. Significant tumor/non-tumor accumulation was observed either by animal sacrification or imaging. [⁶¹Cu]ATSM is a positron emission tomography (PET) radiotracer for tumor hypoxia imaging.

Keywords: radiopharmaceuticals, copper-61, [⁶¹Cu]ATSM, hypoxia, positron emission tomography, fibrosarcoma, imaging